OICR-9429 |
| Katalog-Nr.GC16397 |
OICR-9429 ist ein Inhibitor der WD-Repeat-DomÄne 5 (WDR5) mit hoher AffinitÄt, der die WDR5-Interaktion mit dem MLL-Protein kompetitiv blockiert, indem er die zentrale Peptidbindungstasche von WDR5 bindet. OICR-9429 kann die Histon-H3K4-Trimethylierung unterdrÜcken und kann fÜr die Erforschung verschiedener Krebsarten verwendet werden, darunter nicht-MLL-rearrangierte LeukÄmie, Dickdarm-, BauchspeicheldrÜsen-, Prostatakrebs und Blasenkrebs (BCa) .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1801787-56-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: 5 uM
OICR-9429 is an antagonist of Wdr5-MLL interaction.
WDR5 has been identified as a component of the MLL complex, which is required for histone H3 tri-methylation by its binding of histone H3. Thus, WDR5 is reported to be a presenter component of MLL, suggesting that WDR5 can bind substrates of methylated histone H3 to the MLL complex for further methylation.
In vitro: Previous study found that Wdr5 could be detected readily in C/EBPα immunoprecipitates from lysates of Cebpap30/p30 cells by the treatment of OICR-9429, indicating that the Wdr5-MLL interaction could not influence p30 binding. Moreover, the gene expression profiling of OICR-9429-treated Cebpap30/p30 cells showed that Wdr5 antagonism could result in the upregulation of myeloid-specific transcripts. In addition, the gene set enrichment analyses demonstrated a close correlation between OICR-9429–induced genes and genes that were upregulated after Wdr5 knockdown. Furthermore, the gene profile of Cebpap30/p30 LICs6 was downregulated due to the Wdr5 antagonism caused by OICR-9429. Further treatment of OICR-9429 to Cebpap30/p30 cells was found to be associated with myeloid differentiation and loss of progenitor morphology [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, OICR-9429 is still in the preclinical development stage.
Reference:
[1] Grebien F et al. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol.2015 Aug;11(8):571-8.
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *